53173-91-4

Upstream product

• 2103-94-8 4-(4-bromophenyl)-1,3-thiazol-2-amine 
• 108-24-7 acetic anhydride 
• 127-09-3 sodium acetate 
• 99-90-1 para-bromoacetophenone 
• 99-73-0 para-bromophenacyl bromide 
• 42056-64-4 [4-(4-bromophenyl)-1,3-thiazol-2-yl]amine hydrobromide 

Downstream Products

• 4924-18-9 N-[5-benzoimidazol-1-ylmethyl-4-(4-bromo-phenyl)-thiazol-2-yl]-acetamide 
• 4582-36-9 N-[4-(4-bromo-phenyl)-5-(2-methyl-benzoimidazol-1-ylmethyl)-thiazol-2-yl]-acetamide 
• 4582-35-8 N-[5-(N-benzyl-anilinomethyl)-4-(4-bromo-phenyl)-thiazol-2-yl]-acetamide 
• 4678-83-5 N-[4-(4-bromo-phenyl)-5-(dimethylamino-methyl)-thiazol-2-yl]-acetamide 
• 4588-11-8 N-[4-(4-bromo-phenyl)-5-(diethylamino-methyl)-thiazol-2-yl]-acetamide 
• 4582-34-7 N-[4-(4-bromo-phenyl)-5-(N-methyl-anilinomethyl)-thiazol-2-yl]-acetamide 
• 73034-87-4 5-(2-acetylamino-thiazol-4-yl)-2-bromo-benzenesulfonyl chloride 
• 14269-42-2 N-[5-Bromo-4-(4-bromo-phenyl)-thiazol-2-yl]-acetamide 
• 73034-91-0 5-(2-acetylamino-thiazol-4-yl)-2-bromo-benzenesulfonamide 
• 73034-72-7 5-(2-amino-thiazol-4-yl)-2-bromo-N-phenyl-benzenesulfonamide 
• 73034-73-8 5-(2-amino-thiazol-4-yl)-2-bromo-N-p-tolyl-benzenesulfonamide 
• 73034-76-1 5-(2-amino-thiazol-4-yl)-2-bromo-N-(4-chloro-phenyl)-benzenesulfonamide 
• 73035-07-1 5-(2-amino-thiazol-4-yl)-2-bromo-N-(4-bromo-phenyl)-benzenesulfonamide 
• 73034-74-9 5-(2-amino-thiazol-4-yl)-2-bromo-N-m-tolyl-benzenesulfonamide 

Relevant academic research and scientific papers

2-amino-4-arylthiazole derivatives as anti-giardial agents: Synthesis, biological evaluation and QSAR studies

A series of seven 2-amino-4-arylthiazoles were prepared following Hantzsch's modified method under microwave irradiation. A set of 50 derivatives was obtained and the in vitro activity against Giardia intestinalis was evaluated. The results on the biological activity revealed that, in general, the N-(5-bromo-4-aryl-thiazol-2-yl)-acetamide scaffold showed high bioactivity. In particular, compounds 6e (IC50= 0.39 μM) and 6b (IC50= 0.87 μM) were found to be more potent than the positive control metronidazole. Citoxicity and acute toxicity tests performed showed low toxicity and high selectivity of the most active compounds (6e SI = 139, 6b SI = 52.3). A QSAR analysis was applied to a data set of 37 obtained 2-amino-4-arylthiazoles derivatives and the best model described a strongly correlation between the anti-giardiasic activity and molecular descriptors as E2M, RDF115m, F10, MATS6v, and Hypnotic-80, with high statistical quality. This finding indicates that N-substituted aminothiazole scaffold should be investigated for the development of highly selective anti-giardial agent.

1H-PYROLLO[3,2-d]PYRIMIDINEDIONE DERIVATIVES

The present invention relates to pyrimidinedione compounds of formula (I), salts thereof, to pharmaceutical compositions containing them and their use in medicine. In particular, the invention relates to compounds of formula (I) or salts thereof as activa

Preparation, antimicrobial activity, and toxicity of 2-amino-4-arylthiazole derivatives

Seven 2-amino-4-aryl-1,3-thiazoles (1a-g) and their corresponding 2-aminoacetyl (2a-g) and 2-aminoacetyl-5-bromo (3a-g) derivatives were synthesized and tested in vitro against 11 reference strains, three Gram-positive and four Gram-negative bacteria, two yeasts, and two moulds. Toxicity of the compounds was also evaluated using the brine shrimp test. Compounds 1a, 1b, 1e-g, and 3b showed moderate antimicrobial activity at different concentrations. The results indicated that acetylation of the amino group and bromination at position 5 of the thiazole moiety cause lost of activity. Compounds 1a, 1e, and 1f showed toxicity to brine shrimp nauplii below 10 ppm. Most other compounds showed moderate toxicity, LD50 above 100 ppm. Structures of all compounds were confirmed by NMR and MS data.

Ac2O-Py/basic alumina as a versatile reagent for acetylations in solvent-free conditions under microwave irradiation

Acetic anhydride-pyridine over basic alumina has been used in order to carry out acetylations of hydroxy, thiol and amino groups in solvent-free conditions under microwave irradiation. The technique can be extended for selective acetylations by regulation of irradiation time.